WO2004091494A3 - Method for preparation of site-specific protein conjugates - Google Patents

Method for preparation of site-specific protein conjugates Download PDF

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Publication number
WO2004091494A3
WO2004091494A3 PCT/US2004/010995 US2004010995W WO2004091494A3 WO 2004091494 A3 WO2004091494 A3 WO 2004091494A3 US 2004010995 W US2004010995 W US 2004010995W WO 2004091494 A3 WO2004091494 A3 WO 2004091494A3
Authority
WO
WIPO (PCT)
Prior art keywords
polymer
site
conjugate
protein
preparation
Prior art date
Application number
PCT/US2004/010995
Other languages
French (fr)
Other versions
WO2004091494A2 (en
Inventor
Kenneth Hinds
Danny Lewis
Paul Schmidt
Kathleen M Campbell
Original Assignee
Pr Pharmaceuticals Inc
Kenneth Hinds
Danny Lewis
Paul Schmidt
Kathleen M Campbell
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pr Pharmaceuticals Inc, Kenneth Hinds, Danny Lewis, Paul Schmidt, Kathleen M Campbell filed Critical Pr Pharmaceuticals Inc
Priority to EP04759347.0A priority Critical patent/EP1613272B1/en
Priority to US10/553,570 priority patent/US9040664B2/en
Priority to CA2521381A priority patent/CA2521381C/en
Priority to AU2004229461A priority patent/AU2004229461A1/en
Priority to BR122016021907A priority patent/BR122016021907B8/en
Priority to BRPI0409322A priority patent/BRPI0409322B8/en
Priority to JP2006509863A priority patent/JP2006522816A/en
Publication of WO2004091494A2 publication Critical patent/WO2004091494A2/en
Publication of WO2004091494A3 publication Critical patent/WO2004091494A3/en
Priority to AU2010212312A priority patent/AU2010212312B2/en
Priority to US14/691,855 priority patent/US9789196B2/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/28Insulins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/62Insulins

Abstract

The invention is directed to a single-step method for rapidly and efficiently preparing protein-polymer conjugates, including an insulin-polymer conjugate. According to the method of the present invention, a protein and hydrophilic polymer are contacted in the presence of at least one organic solvent and at least one metal chelator, under conditions that promote the formation of a conjugate of the protein and polymer. Thus, the invention is directed to the site-specific modification of selected proteins, such as insulin, with poly(ethylene glycol) at residue PheB 1. The invention also provides a pharmaceutical formulation for encapsulating the conjugate in a biodegradable polymer.
PCT/US2004/010995 2003-04-11 2004-04-08 Method for preparation of site-specific protein conjugates WO2004091494A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
EP04759347.0A EP1613272B1 (en) 2003-04-11 2004-04-08 Method for preparation of site-specific protein conjugates
US10/553,570 US9040664B2 (en) 2003-04-11 2004-04-08 Materials and methods for preparing protein-polymer conjugates
CA2521381A CA2521381C (en) 2003-04-11 2004-04-08 Method for preparation of site-specific protein conjugates
AU2004229461A AU2004229461A1 (en) 2003-04-11 2004-04-08 Method for preparation of site-specific protein conjugates
BR122016021907A BR122016021907B8 (en) 2003-04-11 2004-04-08 insulin-peg conjugate, poly(lactideco-glycolide) microsphere, drug release formulation, and usage
BRPI0409322A BRPI0409322B8 (en) 2003-04-11 2004-04-08 method for preparing an insulin-polymer conjugate
JP2006509863A JP2006522816A (en) 2003-04-11 2004-04-08 Method for preparing site-specific protein conjugates
AU2010212312A AU2010212312B2 (en) 2003-04-11 2010-08-12 Method for preparation of site-specific protein conjugates
US14/691,855 US9789196B2 (en) 2003-04-11 2015-04-21 Site-specific insulin-polymer conjugates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46236403P 2003-04-11 2003-04-11
US60/462,364 2003-04-11

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US10/553,570 A-371-Of-International US9040664B2 (en) 2003-04-11 2004-04-08 Materials and methods for preparing protein-polymer conjugates
US14/691,855 Division US9789196B2 (en) 2003-04-11 2015-04-21 Site-specific insulin-polymer conjugates

Publications (2)

Publication Number Publication Date
WO2004091494A2 WO2004091494A2 (en) 2004-10-28
WO2004091494A3 true WO2004091494A3 (en) 2006-02-09

Family

ID=33299938

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/010995 WO2004091494A2 (en) 2003-04-11 2004-04-08 Method for preparation of site-specific protein conjugates

Country Status (9)

Country Link
US (2) US9040664B2 (en)
EP (2) EP2599502B1 (en)
JP (3) JP2006522816A (en)
CN (2) CN101514223B (en)
AU (2) AU2004229461A1 (en)
BR (2) BRPI0409322B8 (en)
CA (2) CA3074393A1 (en)
DK (1) DK2599502T3 (en)
WO (1) WO2004091494A2 (en)

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US11590235B2 (en) 2013-09-08 2023-02-28 Kodiak Sciences Inc. Factor VIII zwitterionic polymer conjugates

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CA2532302C (en) 2003-07-15 2016-12-20 Pr Pharmaceuticals, Inc. Method for the preparation of controlled release formulations
BRPI0412211A (en) 2003-07-23 2006-08-22 Pr Pharmaceuticals Inc controlled release compositions
SI1648933T1 (en) * 2003-07-25 2010-01-29 Conjuchem Biotechnologies Inc Long lasting insulin derivatives and methods thereof
WO2005039641A2 (en) * 2003-10-15 2005-05-06 The Regents Of The University Of California Biomacromolecule polymer conjugates
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JP5528710B2 (en) * 2006-02-28 2014-06-25 オリガシス コーポレイション Polymer conjugate containing acryloyloxyethyl phosphorylcholine and process for producing the same
US8394921B2 (en) * 2006-07-25 2013-03-12 Lipoxen Technologies Limited N-terminal derivatisation of proteins with polysaccharides
CA2659990C (en) * 2006-08-04 2016-03-22 Prolong Pharmaceuticals, Inc. Polyethylene glycol erythropoietin conjugates
TWI451876B (en) 2008-06-13 2014-09-11 Lilly Co Eli Pegylated insulin lispro compounds
WO2010030366A2 (en) 2008-09-11 2010-03-18 Nektar Therapeutics Polymeric alpha-hydroxy aldehyde and ketone reagents and conjugation method
EP2350118B1 (en) 2008-09-19 2016-03-30 Nektar Therapeutics Carbohydrate-based drug delivery polymers and conjugates thereof
CN102369209B (en) * 2009-03-20 2015-06-10 韩美科学株式会社 Method for preparing a site-specific physiologically active polypeptide conjugate
GB0905555D0 (en) * 2009-03-31 2009-05-13 Peptcell Ltd Pharmaceutical agent
IN2012DN00407A (en) 2009-08-05 2015-08-21 Pieris Ag
TW201138831A (en) * 2009-09-30 2011-11-16 Prolong Pharmaceuticals Inc Modified granulocyte colony stimulating factor (G-CSF)
US8765432B2 (en) 2009-12-18 2014-07-01 Oligasis, Llc Targeted drug phosphorylcholine polymer conjugates
AR081066A1 (en) 2010-04-02 2012-06-06 Hanmi Holdings Co Ltd INSULIN CONJUGATE WHERE AN IMMUNOGLOBULIN FRAGMENT IS USED
US9981017B2 (en) 2010-04-02 2018-05-29 Hanmi Science Co., Ltd. Insulin conjugate using an immunoglobulin fragment
KR20130049671A (en) * 2011-11-04 2013-05-14 한미사이언스 주식회사 Method for preparation of biological active polypeptide conjugate
AR090281A1 (en) * 2012-03-08 2014-10-29 Hanmi Science Co Ltd IMPROVED PROCESS FOR THE PREPARATION OF A PHYSIOLOGICALLY ACTIVE POLYPEPTIDE COMPLEX
AR090843A1 (en) 2012-05-09 2014-12-10 Lilly Co Eli TREATMENT FOR DIABETES COMORBID WITH CHRONIC RENAL DISEASE
WO2014029012A1 (en) * 2012-08-23 2014-02-27 Stemcell Technologies Inc. Compositions and methods for rapid and reversible biomolecular labeling
US10188739B2 (en) 2014-02-27 2019-01-29 Xenetic Biosciences, Inc. Compositions and methods for administering insulin or insulin-like protein to the brain
US9840553B2 (en) 2014-06-28 2017-12-12 Kodiak Sciences Inc. Dual PDGF/VEGF antagonists
US9439864B2 (en) * 2014-07-07 2016-09-13 Antriabio, Inc. Solvent extraction from biodegradable microparticles
JP2017525370A (en) 2014-08-21 2017-09-07 ザ ジェネラル ホスピタル コーポレイション Tumor necrosis factor superfamily and TNF-like ligand muteins and methods of preparing and using tumor necrosis factor superfamily and TNF-like ligand muteins
KR20210013299A (en) 2014-10-17 2021-02-03 코디악 사이언시스 인코포레이티드 Butyrylcholinesterase zwitterionic polymer conjugates
US20160151511A1 (en) * 2014-12-02 2016-06-02 Antriabio, Inc. Proteins and protein conjugates with increased hydrophobicity
WO2016196017A1 (en) 2015-06-04 2016-12-08 Antriabio, Inc. Amine pegylation methods for the preparation of site-specific protein conjugates
RU2744860C2 (en) 2015-12-30 2021-03-16 Кодиак Сайенсиз Инк. Antibodies and their conjugates
CA3157509A1 (en) 2019-10-10 2021-04-15 Kodiak Sciences Inc. Methods of treating an eye disorder

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Publication number Priority date Publication date Assignee Title
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Also Published As

Publication number Publication date
BRPI0409322B8 (en) 2021-05-25
AU2010212312A1 (en) 2010-09-02
CA3074393A1 (en) 2004-10-28
EP1613272A2 (en) 2006-01-11
WO2004091494A2 (en) 2004-10-28
US9040664B2 (en) 2015-05-26
BR122016021907B8 (en) 2021-07-27
CN101514223B (en) 2017-03-01
BR122016021907B1 (en) 2018-01-09
CA2521381C (en) 2020-05-26
EP2599502A2 (en) 2013-06-05
JP2010248241A (en) 2010-11-04
CA2521381A1 (en) 2004-10-28
EP1613272B1 (en) 2013-12-18
US20150216995A1 (en) 2015-08-06
US9789196B2 (en) 2017-10-17
EP2599502A3 (en) 2014-07-30
JP5576200B2 (en) 2014-08-20
EP2599502B1 (en) 2017-03-01
BRPI0409322A (en) 2006-04-25
EP1613272A4 (en) 2010-06-16
AU2010212312B2 (en) 2012-05-17
US20070083006A1 (en) 2007-04-12
AU2004229461A1 (en) 2004-10-28
DK2599502T3 (en) 2017-04-18
CN1777440A (en) 2006-05-24
CN101514223A (en) 2009-08-26
JP2006522816A (en) 2006-10-05
BRPI0409322B1 (en) 2017-02-07
JP2013256498A (en) 2013-12-26

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